186re -头孢克肟作为细菌感染潜在诊断和治疗药物的制备

H. Talaat, M. Aydia, I. T. Ibrahim, H. El-Said, K. M. El-Azony
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引用次数: 1

摘要

研究了影响186re -头孢克肟制备的几个因素,如头孢克肟和氯化亚锡的用量、pH、反应时间和反应温度,以优化标记条件,以获得186re -头孢克肟放射化学产率最高。采用纸层析法测定铼-186的放射化学纯度,采用电泳和高效液相色谱法测定186re -头孢克肟的放射化学产率和纯度。采用2mg头孢克肟,0.3mg载体加入186Re和0.5mg氯化亚锡,pH为5.5,室温下30min,获得186Re-头孢克肟的最大放射化学产率(96±2.8%)。对正常小鼠、无菌感染小鼠和细菌感染小鼠进行生物分布。结果表明,186re -头孢克肟在细菌感染肌肉(脓毒性炎症)中的浓度高于无菌感染肌肉(无菌性炎症)。因此,186re -头孢克肟可用于区分感染性炎症和无菌性炎症。
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Preparation of 186Re-Cefixime as a Potential Diagnostic and Therapeutic Agent for Bacterial Infection
SEVERAL factors that influence the preparation of 186Re-Cefixime such as the amount of Cefixime and stannous chloride, pH, reaction time and reaction temperature were studied to optimize the labeling conditions to obtain the highest radiochemical yield of 186Re-Cefixime. The radiochemical purity of Rhenium-186 was determined by paper chromatography, while the radiochemical yield and purity of 186Re-Cefixime were determined by electrophoresis and high-performance liquid chromatography (HPLC). The maximum radiochemical yield of 186Re-Cefixime was obtained (96±2.8%) using 2mg Cefixime, 0.3mg carrier added 186Re and 0.5mg stannous chloride at pH 5.5, within 30min at room temperature. The bio-distribution was carried out on three types of mice (normal, sterile infected and bacterial infected). The results show that 186Re-Cefixime is more concentrated in the bacterially infected muscle (septic inflammation) than in the sterile infected muscle (aseptic inflammation). Therefore, 186Re-Cefixime could be used to differentiate between septic and aseptic inflammation.
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